E0814New |
Masitinib mesylate
|
Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit with IC50 of 200 nM for human recombinant c-Kit, also inhibits PDGFRα/β with IC50s of 540/800 nM, Lyn with IC50 of 510 nM for LynB, and, to a lesser extent, FGFR3 and FAK. |
|
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S0278 |
SU5614
|
SU5614 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. SU5614 reduces cell proliferation and induces apoptosis. |
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Adv Sci (Weinh), 2021, e2101848
-
Front Cell Dev Biol, 2021, 9:797047
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S0377 |
CS-2660 (JNJ-38158471)
|
CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such as RET (c-RET) and Kit (c-Kit) with IC50 of 180 nM and 500 nM,while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3. |
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S0504 |
SU14813
|
SU14813 (SU 014813) is a multiple receptor tyrosine kinase inhibitor with IC50 of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and Kit (c-Kit). SU14813 exhibits potent antiangiogenic and antitumor activity. |
-
Adv Sci (Weinh), 2021, e2101848
|
|
S1005 |
Axitinib (AG 013736)
|
Axitinib (AG 013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively. |
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Cancer Cell, 2022, S1535-6108(21)00662-0
-
Sci Adv, 2022, 8(6):eabg9455
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Sci Adv, 2022, 8(2):eabi8683
|
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S1017 |
Cediranib (AZD2171)
|
Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3. |
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Mol Cancer Ther, 2022, 21(6):1030-1043
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Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Cell Rep Med, 2022, 3(1):100492
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S1018 |
Dovitinib (TKI-258)
|
Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4. |
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Cell Rep Med, 2022, 3(1):100492
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Mol Cell, 2021, S1097-2765(21)00507-4
-
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
|
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S1021 |
Dasatinib (BMS-354825)
|
Dasatinib (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity. |
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Cancer Cell, 2022, S1535-6108(21)00662-0
-
J Immunother Cancer, 2022, 10(1)e003766
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Cancer Res, 2022, canres.1823.2021
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S1026 |
Imatinib (STI571) Mesylate
|
Imatinib (STI571, CGP057148B, Gleevec) Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy. |
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Cell Metab, 2022, S1550-4131(22)00131-0
-
Signal Transduct Target Ther, 2022, 7(1):33
-
Sci Adv, 2022, 8(6):eabg9455
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S1032 |
Motesanib Diphosphate (AMG-706)
|
Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit (c-Kit), ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3. |
-
Front Cell Dev Biol, 2022, 10:836179
-
Drug Metab Dispos, 2021, 49(1):53-61
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Cell Stem Cell, 2019, 25(1):69-86
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S1035 |
Pazopanib HCl (GW786034 HCl)
|
Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death. |
-
NPJ Breast Cancer, 2022, 8(1):44
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Cancer Cell, 2021, S1535-6108(21)00659-0
|
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S1040 |
Sorafenib (BAY 43-9006) tosylate
|
Sorafenib (BAY 43-9006) tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. |
-
Cancer Cell, 2022, S1535-6108(21)00662-0
-
Bioact Mater, 2022, 18:459-470
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Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
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S1042 |
Sunitinib (SU11248) malate
|
Sunitinib (SU11248) malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis. |
-
Clin Cancer Res, 2022, clincanres.4291.2021
-
NPJ Breast Cancer, 2022, 8(1):44
-
Cancers (Basel), 2022, 14(7)1639
|
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S1064 |
Masitinib (AB1010)
|
Masitinib is a novel inhibitor for Kit (c-Kit) and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3. |
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Haematologica, 2022, 10.3324/haematol.2021.279957
-
Vet Comp Oncol, 2022, 10.1111/vco.12817
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Cell Chem Biol, 2021, S2451-9456(21)00303-2
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S1111 |
Foretinib (GSK1363089)
|
Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2. |
-
Int J Mol Sci, 2022, 23(2)775
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Cell Rep Med, 2022, 3(1):100492
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S1164 |
Lenvatinib (E7080)
|
Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3. |
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Cell Rep, 2022, 39(3):110712
-
Cell Death Dis, 2022, 13(4):351
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Clin Transl Med, 2022, 12(1):e662
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S1178 |
Regorafenib (BAY 73-4506)
|
Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy. |
-
Cancer Cell, 2022, S1535-6108(21)00662-0
-
Cell Rep, 2022, 39(3):110712
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Cell Rep, 2022, 38(10):110490
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S1207 |
Tivozanib (AV-951)
|
Tivozanib (AV-951, KRN-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3. |
-
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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Hum Cell, 2021, 10.1007/s13577-021-00639-4
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S1220 |
OSI-930
|
OSI-930 is a potent inhibitor of Kit (c-Kit), KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1. |
-
Cell Rep, 2019, 28(9):2331-2344
-
Nat Biomed Eng, 2018, 2(8):578-588
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Mol Syst Biol, 2015, 11(1):789
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|
S1244 |
Amuvatinib (MP-470)
|
Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
mBio, 2021, 12(6):e0322821
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Hum Cell, 2021, 34(6):1911-1918
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|
S1363 |
Ki8751
|
Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR. |
-
Front Oncol, 2021, 11:650052
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J Clin Med, 2020, 9(3)
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Front Pharmacol, 2020, 11:572624
|
|
S2070 |
ISCK03
|
ISCK03 (N-(4-imidazol-1-yl phenyl)sulfonamide) is a cell-permeable inhibitor of stem-cell factor (SCF)/c-kit signaling.ISCK03 inhibits SCF-induced c-c-kit phosphorylation and downstream ERK phosphorylation. |
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S2231 |
Telatinib
|
Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2. |
-
Sci Adv, 2022, 8(6):eabg9455
-
Leiden University Scholarly Publications, 2020, N/A
-
Cell Stem Cell, 2019, 24(4):654-669
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S2475 |
Imatinib (STI571)
|
Imatinib (STI571, CGP057148B, Gleevec) is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy. |
-
Cell, 2022, S0092-8674(22)00472-X
-
Sci Adv, 2022, 8(6):eabg9455
-
Cell Rep, 2022, 39(4):110721
|
|
S3012 |
Pazopanib
|
Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy. |
-
NPJ Breast Cancer, 2022, 8(1):44
-
J Pharmacol Exp Ther, 2022, 380(2):114-125
-
Birth Defects Res, 2022, 10.1002/bdr2.2001
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S4001 |
Cabozantinib malate
|
Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis. |
-
Adv Sci (Weinh), 2022, e2201478
-
Cancer Res, 2022, canres.1397.2021
-
Cancers (Basel), 2022, 14(7)1683
|
|
S4947 |
Regorafenib Hydrochloride
|
Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. |
-
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
-
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
-
Front Oncol, 2021, 11:796839
|
|
S5077 |
Regorafenib (BAY-734506) Monohydrate
|
Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively. |
-
Pharmazie, 2022, 77(2):54-58
-
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
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Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
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S5240 |
Lenvatinib (E7080) Mesylate
|
Lenvatinib Mesylate (E7080) is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity. |
-
Cell Death Dis, 2022, 13(4):351
-
Clin Transl Med, 2022, 12(1):e662
-
Pharmazie, 2022, 77(2):54-58
|
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S6662 |
AST-487 (NVP-AST487)
|
AST-487 (NVP-AST487), a N,N'-diphenyl urea,is an ATP competitive inhibitor of Flt3 with ki of 0.12 μM.Besides FLT3, AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM. |
-
Nat Commun, 2020, 21;11(1):1924
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|
S7003 |
AZD2932
|
AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
|
-
Cancer Res, 2020, canres.1992.2020
-
Molecules, 2020, 8;25(9) pii: E2220
-
Development, 2016, 143(23):4394-4404
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S7688 |
Ki20227
|
Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively. |
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S7765 |
Dovitinib (TKI258) Lactate
|
Dovitinib (TKI258, CHIR258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
|
-
Mol Cell, 2021, S1097-2765(21)00507-4
-
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
-
Cancer Res, 2021, canres.1780.2020
|
|
S7781 |
Sunitinib (SU11248)
|
Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis. |
-
Mol Cell, 2022, S1097-2765(22)00105-8
-
Clin Cancer Res, 2022, clincanres.4291.2021
-
Cell Rep, 2022, 39(5):110750
|
|
S7782 |
Dasatinib Monohydrate
|
Dasatinib Monohydrate (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
|
-
NPJ Precis Oncol, 2022, 6(1):16
-
Front Immunol, 2022, 13:841045
-
Anal Chem, 2022, 10.1021/acs.analchem.1c05455
|
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S7818 |
Pexidartinib (PLX3397)
|
Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3. |
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J Clin Invest, 2022, 132(3)e145071
-
Aging Cell, 2022, 10.1111/acel.13623
-
Int J Mol Sci, 2022, 23(5)2793
|
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S8015 |
Agerafenib (RXDX-105)
|
Agerafenib (RXDX-105, CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2. |
-
Mol Pharmacol, 2021, 99(6):435-447
-
Dis Model Mech, 2020, dmm.047779
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Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520
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S8024 |
Tyrphostin AG 1296
|
Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. Tyrphostin AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. Tyrphostin AG1296 induces dramatic apoptosis in A375R cells. |
-
Front Pharmacol, 2021, 12:804327
-
J Cardiovasc Dev Dis, 2021, 8(3)28
-
Mol Med Rep, 2021, 23(4):1
|
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S8401 |
Erdafitinib (JNJ-42756493)
|
Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis. |
-
JCI Insight, 2022, 7(7)e154824
-
Oncoimmunology, 2022, 11(1):2021619
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
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S8553 |
Avapritinib (BLU-285)
|
Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous Kit (c-Kit) mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM). |
-
Sci Adv, 2022, 8(6):eabg9455
-
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
-
JCI Insight, 2020, 143474
|
|
S8573 |
Sitravatinib (MGCD516)
|
Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl. |
-
Cancers (Basel), 2021, 13(21)5474
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Cancers (Basel), 2020, 12(1)
|
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S8721 |
PDGFR inhibitor 1
|
PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of Kit (c-Kit) and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth. |
-
Oncogene, 2022, 41(20):2860-2872
|
|
S8757 |
Ripretinib (DCC-2618)
|
DCC-2618 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of the tumor-associated antigens (TAA) mast/stem cell factor receptor (SCFR) Kit (c-Kit) and PDGFR-alpha, with IC50 values of 4 nM, 8 nM, 18 nM, 5 nM and 14 nM for WT Kit (c-Kit), V654A Kit (c-Kit), T670I Kit (c-Kit), D816H Kit (c-Kit) and D816V Kit (c-Kit), respectively. |
-
Cancers (Basel), 2021, 13(15)3699
-
J Pers Med, 2020, 10(4)E234
-
Expert Opin Pharmacother, 2019, 20(13):1539-1550
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S8780 |
AZD3229
|
AZD3229 is a potent, pan-Kit (c-Kit) mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant Kit (c-Kit) driven Ba/F3 cell lines (GI50=1-50 nM), with good margin to KDR-driven effects. It also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V). |
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S9662 |
UNC2025
|
UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively. |
-
JCI Insight, 2022, 7(7)e154824
-
Front Immunol, 2020, 11:564133
-
Cell Signal, 2014, 26(1):149-61
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S9973New |
Flumatinib (HH-GV-678)
|
Flumatinib (HH-GV-678) is a novel inhibitor of Bcr-Abl with IC50 values of 1.2 nM, 307.6 nM and 665.5 nM for c-Abl, PDGFRβand c-Kit, respectively.
|
|
|
E0814New |
Masitinib mesylate
|
Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit with IC50 of 200 nM for human recombinant c-Kit, also inhibits PDGFRα/β with IC50s of 540/800 nM, Lyn with IC50 of 510 nM for LynB, and, to a lesser extent, FGFR3 and FAK. |
|
|
S0278 |
SU5614
|
SU5614 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. SU5614 reduces cell proliferation and induces apoptosis. |
- Adv Sci (Weinh), 2021, e2101848
- Front Cell Dev Biol, 2021, 9:797047
|
|
S0377 |
CS-2660 (JNJ-38158471)
|
CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such as RET (c-RET) and Kit (c-Kit) with IC50 of 180 nM and 500 nM,while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3. |
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S0504 |
SU14813
|
SU14813 (SU 014813) is a multiple receptor tyrosine kinase inhibitor with IC50 of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and Kit (c-Kit). SU14813 exhibits potent antiangiogenic and antitumor activity. |
- Adv Sci (Weinh), 2021, e2101848
|
|
S1005 |
Axitinib (AG 013736)
|
Axitinib (AG 013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively. |
- Cancer Cell, 2022, S1535-6108(21)00662-0
- Sci Adv, 2022, 8(6):eabg9455
- Sci Adv, 2022, 8(2):eabi8683
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S1017 |
Cediranib (AZD2171)
|
Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3. |
- Mol Cancer Ther, 2022, 21(6):1030-1043
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Cell Rep Med, 2022, 3(1):100492
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S1018 |
Dovitinib (TKI-258)
|
Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4. |
- Cell Rep Med, 2022, 3(1):100492
- Mol Cell, 2021, S1097-2765(21)00507-4
- Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
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S1021 |
Dasatinib (BMS-354825)
|
Dasatinib (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity. |
- Cancer Cell, 2022, S1535-6108(21)00662-0
- J Immunother Cancer, 2022, 10(1)e003766
- Cancer Res, 2022, canres.1823.2021
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S1026 |
Imatinib (STI571) Mesylate
|
Imatinib (STI571, CGP057148B, Gleevec) Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy. |
- Cell Metab, 2022, S1550-4131(22)00131-0
- Signal Transduct Target Ther, 2022, 7(1):33
- Sci Adv, 2022, 8(6):eabg9455
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S1032 |
Motesanib Diphosphate (AMG-706)
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Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit (c-Kit), ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3. |
- Front Cell Dev Biol, 2022, 10:836179
- Drug Metab Dispos, 2021, 49(1):53-61
- Cell Stem Cell, 2019, 25(1):69-86
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S1035 |
Pazopanib HCl (GW786034 HCl)
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Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death. |
- NPJ Breast Cancer, 2022, 8(1):44
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Cancer Cell, 2021, S1535-6108(21)00659-0
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S1040 |
Sorafenib (BAY 43-9006) tosylate
|
Sorafenib (BAY 43-9006) tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. |
- Cancer Cell, 2022, S1535-6108(21)00662-0
- Bioact Mater, 2022, 18:459-470
- Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
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S1042 |
Sunitinib (SU11248) malate
|
Sunitinib (SU11248) malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis. |
- Clin Cancer Res, 2022, clincanres.4291.2021
- NPJ Breast Cancer, 2022, 8(1):44
- Cancers (Basel), 2022, 14(7)1639
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S1064 |
Masitinib (AB1010)
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Masitinib is a novel inhibitor for Kit (c-Kit) and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3. |
- Haematologica, 2022, 10.3324/haematol.2021.279957
- Vet Comp Oncol, 2022, 10.1111/vco.12817
- Cell Chem Biol, 2021, S2451-9456(21)00303-2
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S1111 |
Foretinib (GSK1363089)
|
Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2. |
- Int J Mol Sci, 2022, 23(2)775
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Cell Rep Med, 2022, 3(1):100492
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S1164 |
Lenvatinib (E7080)
|
Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3. |
- Cell Rep, 2022, 39(3):110712
- Cell Death Dis, 2022, 13(4):351
- Clin Transl Med, 2022, 12(1):e662
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S1178 |
Regorafenib (BAY 73-4506)
|
Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy. |
- Cancer Cell, 2022, S1535-6108(21)00662-0
- Cell Rep, 2022, 39(3):110712
- Cell Rep, 2022, 38(10):110490
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S1207 |
Tivozanib (AV-951)
|
Tivozanib (AV-951, KRN-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3. |
- Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 10.1007/s13577-021-00639-4
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S1220 |
OSI-930
|
OSI-930 is a potent inhibitor of Kit (c-Kit), KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1. |
- Cell Rep, 2019, 28(9):2331-2344
- Nat Biomed Eng, 2018, 2(8):578-588
- Mol Syst Biol, 2015, 11(1):789
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S1244 |
Amuvatinib (MP-470)
|
Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- mBio, 2021, 12(6):e0322821
- Hum Cell, 2021, 34(6):1911-1918
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S1363 |
Ki8751
|
Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR. |
- Front Oncol, 2021, 11:650052
- J Clin Med, 2020, 9(3)
- Front Pharmacol, 2020, 11:572624
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S2070 |
ISCK03
|
ISCK03 (N-(4-imidazol-1-yl phenyl)sulfonamide) is a cell-permeable inhibitor of stem-cell factor (SCF)/c-kit signaling.ISCK03 inhibits SCF-induced c-c-kit phosphorylation and downstream ERK phosphorylation. |
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S2231 |
Telatinib
|
Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2. |
- Sci Adv, 2022, 8(6):eabg9455
- Leiden University Scholarly Publications, 2020, N/A
- Cell Stem Cell, 2019, 24(4):654-669
|
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S2475 |
Imatinib (STI571)
|
Imatinib (STI571, CGP057148B, Gleevec) is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy. |
- Cell, 2022, S0092-8674(22)00472-X
- Sci Adv, 2022, 8(6):eabg9455
- Cell Rep, 2022, 39(4):110721
|
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S3012 |
Pazopanib
|
Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy. |
- NPJ Breast Cancer, 2022, 8(1):44
- J Pharmacol Exp Ther, 2022, 380(2):114-125
- Birth Defects Res, 2022, 10.1002/bdr2.2001
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S4001 |
Cabozantinib malate
|
Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis. |
- Adv Sci (Weinh), 2022, e2201478
- Cancer Res, 2022, canres.1397.2021
- Cancers (Basel), 2022, 14(7)1683
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S4947 |
Regorafenib Hydrochloride
|
Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. |
- ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
- Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
- Front Oncol, 2021, 11:796839
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S5077 |
Regorafenib (BAY-734506) Monohydrate
|
Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively. |
- Pharmazie, 2022, 77(2):54-58
- ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
- Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
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S5240 |
Lenvatinib (E7080) Mesylate
|
Lenvatinib Mesylate (E7080) is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity. |
- Cell Death Dis, 2022, 13(4):351
- Clin Transl Med, 2022, 12(1):e662
- Pharmazie, 2022, 77(2):54-58
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S6662 |
AST-487 (NVP-AST487)
|
AST-487 (NVP-AST487), a N,N'-diphenyl urea,is an ATP competitive inhibitor of Flt3 with ki of 0.12 μM.Besides FLT3, AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM. |
- Nat Commun, 2020, 21;11(1):1924
|
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S7003 |
AZD2932
|
AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
|
- Cancer Res, 2020, canres.1992.2020
- Molecules, 2020, 8;25(9) pii: E2220
- Development, 2016, 143(23):4394-4404
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S7688 |
Ki20227
|
Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively. |
|
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S7765 |
Dovitinib (TKI258) Lactate
|
Dovitinib (TKI258, CHIR258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
|
- Mol Cell, 2021, S1097-2765(21)00507-4
- Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
- Cancer Res, 2021, canres.1780.2020
|
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S7781 |
Sunitinib (SU11248)
|
Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis. |
- Mol Cell, 2022, S1097-2765(22)00105-8
- Clin Cancer Res, 2022, clincanres.4291.2021
- Cell Rep, 2022, 39(5):110750
|
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S7782 |
Dasatinib Monohydrate
|
Dasatinib Monohydrate (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
|
- NPJ Precis Oncol, 2022, 6(1):16
- Front Immunol, 2022, 13:841045
- Anal Chem, 2022, 10.1021/acs.analchem.1c05455
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S7818 |
Pexidartinib (PLX3397)
|
Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3. |
- J Clin Invest, 2022, 132(3)e145071
- Aging Cell, 2022, 10.1111/acel.13623
- Int J Mol Sci, 2022, 23(5)2793
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S8015 |
Agerafenib (RXDX-105)
|
Agerafenib (RXDX-105, CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2. |
- Mol Pharmacol, 2021, 99(6):435-447
- Dis Model Mech, 2020, dmm.047779
- Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520
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S8024 |
Tyrphostin AG 1296
|
Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. Tyrphostin AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. Tyrphostin AG1296 induces dramatic apoptosis in A375R cells. |
- Front Pharmacol, 2021, 12:804327
- J Cardiovasc Dev Dis, 2021, 8(3)28
- Mol Med Rep, 2021, 23(4):1
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S8401 |
Erdafitinib (JNJ-42756493)
|
Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis. |
- JCI Insight, 2022, 7(7)e154824
- Oncoimmunology, 2022, 11(1):2021619
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
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S8553 |
Avapritinib (BLU-285)
|
Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous Kit (c-Kit) mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM). |
- Sci Adv, 2022, 8(6):eabg9455
- Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
- JCI Insight, 2020, 143474
|
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S8573 |
Sitravatinib (MGCD516)
|
Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl. |
- Cancers (Basel), 2021, 13(21)5474
- Cancers (Basel), 2020, 12(1)
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S8721 |
PDGFR inhibitor 1
|
PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of Kit (c-Kit) and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth. |
- Oncogene, 2022, 41(20):2860-2872
|
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S8757 |
Ripretinib (DCC-2618)
|
DCC-2618 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of the tumor-associated antigens (TAA) mast/stem cell factor receptor (SCFR) Kit (c-Kit) and PDGFR-alpha, with IC50 values of 4 nM, 8 nM, 18 nM, 5 nM and 14 nM for WT Kit (c-Kit), V654A Kit (c-Kit), T670I Kit (c-Kit), D816H Kit (c-Kit) and D816V Kit (c-Kit), respectively. |
- Cancers (Basel), 2021, 13(15)3699
- J Pers Med, 2020, 10(4)E234
- Expert Opin Pharmacother, 2019, 20(13):1539-1550
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S8780 |
AZD3229
|
AZD3229 is a potent, pan-Kit (c-Kit) mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant Kit (c-Kit) driven Ba/F3 cell lines (GI50=1-50 nM), with good margin to KDR-driven effects. It also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V). |
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S9662 |
UNC2025
|
UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively. |
- JCI Insight, 2022, 7(7)e154824
- Front Immunol, 2020, 11:564133
- Cell Signal, 2014, 26(1):149-61
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S9973New |
Flumatinib (HH-GV-678)
|
Flumatinib (HH-GV-678) is a novel inhibitor of Bcr-Abl with IC50 values of 1.2 nM, 307.6 nM and 665.5 nM for c-Abl, PDGFRβand c-Kit, respectively.
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